Synthesis and biological assays of E-ring analogs of camptothecin and homocamptothecin

Analogs of the anti-tumor agent camptothecin with both closed E-rings (lactone and ether) and open E-rings (reduced acid, hydrazide, and protected Weinreb amide) have been prepared and tested in topoisomerase and cellular assays. The results provide insights into the structural features of the campt...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry Vol. 14; no. 18; pp. 6202 - 6212
Main Authors:	Tangirala, Raghuram S., Antony, Smitha, Agama, Keli, Pommier, Yves, Anderson, Bradley D., Bevins, Robert, Curran, Dennis P.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 15-09-2006 Elsevier Science
Subjects:	Anti-cancer agents Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Biological Assay Camptothecin Camptothecin - analogs & derivatives Camptothecin - chemical synthesis Camptothecin - chemistry Camptothecin - pharmacology Cascade radical annulation Cell Line, Tumor Cell Proliferation - drug effects DNA - drug effects Drug Screening Assays, Antitumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Humans Magnetic Resonance Spectroscopy Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments Structure-Activity Relationship Topoisomerase 1 Topoisomerase Inhibitors Camptothecin Topoisomerase 1 Cascade radical annulation Anti-cancer agents Antineoplastic agent Organic hydrazide Ether Enzyme DNA topoisomerase Lactam Amides Lactone In vitro Biological activity Annelation Alkaloid Isomerases Hydroxyacid Cleavage Chemical synthesis
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